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Cryo-EM structure of the human CDK-activating kinase bound to the clinical inhibitor ICEC0942

ABSTRACT:

SUBMITTER: Basil J Greber

PROVIDER: EMPIAR-10561 | biostudies-other |

REPOSITORIES: biostudies-other

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2.5 Å-resolution structure of human CDK-activating kinase bound to the clinical inhibitor ICEC0942.

Greber Basil J BJ Remis Jonathan J Ali Simak S Nogales Eva E

Biophysical journal 20210119 4

The human CDK-activating kinase (CAK), composed of CDK7, cyclin H, and MAT1, is involved in the control of transcription initiation and the cell cycle. Because of these activities, it has been identified as a promising target for cancer chemotherapy. A number of CDK7 inhibitors have entered clinical trials, among them ICEC0942 (also known as CT7001). Structural information can aid in improving the affinity and specificity of such drugs or drug candidates, reducing side effects in patients. Here, ...[more]

PMID: 33476598

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